1. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  2. PROTACs c-Met/HGFR Apoptosis
  3. PRO-6E

PRO-6E 是一种具有口服活性的以 Cereblon 配体为基础的 PROTAC,可以降解 MET,在 1 μM 的浓度下对 MKN-45 细胞中 MET 的最大降解率为 81.9% 。PRO-6E 在体内外抑制肿瘤生长。PRO-6E 可以诱导细胞凋亡 (apoptosis) 和细胞周期阻滞(结构备注:(Blue: Cereblon 配体 (HY-103596), Black: linker;Pink: ALK/c-Met 抑制剂 Crizotinib (HY-50878))。

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PRO-6E Chemical Structure

PRO-6E Chemical Structure

CAS No. : 2353493-69-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥12436
In-stock
1 mg ¥2900
In-stock
5 mg ¥6660
In-stock
10 mg   询价  
50 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker;Pink: ALK/c-Met inhibitor Crizotinib (HY-50878))[1].

体外研究
(In Vitro)

PRO-6E (0.03-10 μM; 48 h) 对 MKN-45、SNU-638 细胞生长的抑制作用[1]
PRO-6E (1 μM; 超过24 h) 促进 MKN-45 细胞 MET 降解[1]
PRO-6E (0.1-1 μM; 48 h) 使 MKN-45 细胞中 G2/M 相细胞百分比增加,S 相细胞百分比减少[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MKN-45, SNU-638 cells
Concentration: 0, 0.03, 0.1, 0.3, 1, 3, 10 μM
Incubation Time: 48 h
Result: Inhibited the cell growth.

Cell Cycle Analysis[1]

Cell Line: MKN-45 cells
Concentration: 0, 0.1, 0.3, 1, 3 μM
Incubation Time: 48 h
Result: Increased in the percentage of G2/M phase cells and decreased in the percentage of S phase cells.

Western Blot Analysis[1]

Cell Line: MKN-45 cells
Concentration: 0, 0.03, 0.1, 0.3, 1, 3 μM
Incubation Time: 12, 24, 36, 48, and 72 h
Result: facilitated MET degradation over 24 hours.
体内研究
(In Vivo)

PRO-6E (口服; 30 mg/kg/天; 持续15天) 抑制 MKN - 45 细胞来源的异种移植肿瘤模型的肿瘤生长[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MKN‐45 cell‐derived xenograft tumor model[1]
Dosage: 30 mg/kg/day for 15 days
Administration: Oral gavage
Result: Inhibited tumor growth.
分子量

848.75

Formula

C42H44Cl2FN7O7

CAS 号
性状

固体

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 100 mg/mL (117.82 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.1782 mL 5.8910 mL 11.7820 mL
5 mM 0.2356 mL 1.1782 mL 2.3564 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.1782 mL 5.8910 mL 11.7820 mL 29.4551 mL
5 mM 0.2356 mL 1.1782 mL 2.3564 mL 5.8910 mL
10 mM 0.1178 mL 0.5891 mL 1.1782 mL 2.9455 mL
15 mM 0.0785 mL 0.3927 mL 0.7855 mL 1.9637 mL
20 mM 0.0589 mL 0.2946 mL 0.5891 mL 1.4728 mL
25 mM 0.0471 mL 0.2356 mL 0.4713 mL 1.1782 mL
30 mM 0.0393 mL 0.1964 mL 0.3927 mL 0.9818 mL
40 mM 0.0295 mL 0.1473 mL 0.2946 mL 0.7364 mL
50 mM 0.0236 mL 0.1178 mL 0.2356 mL 0.5891 mL
60 mM 0.0196 mL 0.0982 mL 0.1964 mL 0.4909 mL
80 mM 0.0147 mL 0.0736 mL 0.1473 mL 0.3682 mL
100 mM 0.0118 mL 0.0589 mL 0.1178 mL 0.2946 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
PRO-6E
目录号:
HY-160506
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